Assay Detail
Binding
CHEMBL1012740
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DPCPX from bovine brain cortical membrane adenosine A1 receptor
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Pyrido[2,3-e]-1,2,4-triazolo[4,3-a]pyrazin-1-one as a new scaffold to develop potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 7.41 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473648 | — | — | 1 | 9.42 |
| CHEMBL473649 | — | — | 1 | 9.33 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | — | 1 | 9.30 |
| CHEMBL474636 | — | — | 1 | 8.51 |
| CHEMBL379791 | — | — | 1 | 8.22 |
| CHEMBL473839 | — | — | 1 | 8.15 |
| CHEMBL514156 | — | — | 1 | 7.85 |
| CHEMBL516372 | — | — | 1 | 7.15 |
| CHEMBL514155 | — | — | 1 | 6.95 |
| CHEMBL514196 | — | — | 1 | 6.84 |
| CHEMBL473650 | — | — | 1 | 6.82 |
| CHEMBL515433 | — | — | 1 | 6.74 |
| CHEMBL475792 | — | — | 1 | 6.51 |
| CHEMBL474016 | — | — | 1 | 6.45 |
| CHEMBL473634 | — | — | 1 | 6.35 |
| CHEMBL474977 | — | — | 1 | 5.96 |
| CHEMBL1355736 | THEOPHYLLINE | 4.0 | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473648 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL473649 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL183 | 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL474636 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL379791 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL473839 | — | Ki | = | 7.15 | nM | 8.15 |
| CHEMBL514156 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL516372 | — | Ki | = | 70.7 | nM | 7.15 |
| CHEMBL514155 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL514196 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL473650 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL515433 | — | Ki | = | 181.0 | nM | 6.74 |
| CHEMBL475792 | — | Ki | = | 305.5 | nM | 6.51 |
| CHEMBL474016 | — | Ki | = | 355.0 | nM | 6.45 |
| CHEMBL473634 | — | Ki | = | 449.0 | nM | 6.35 |
| CHEMBL474977 | — | Ki | = | 1102.0 | nM | 5.96 |
| CHEMBL1355736 | THEOPHYLLINE | Ki | = | 3800.0 | nM | 5.42 |